[HTML][HTML] Extracellular ionic locks determine variation in constitutive activity and ligand potency between species orthologs of the free fatty acid receptors FFA2 and …

…, IG Tikhonova, SK Pandey, T Ulven, G Milligan - Journal of Biological …, 2012 - ASBMB
Free fatty acid receptors 2 and 3 (FFA2 and FFA3) are G protein-coupled receptors for short
chain free fatty acids (SCFAs). They respond to the same set of endogenous ligands but with …

Discovery of novel agonists and antagonists of the free fatty acid receptor 1 (FFAR1) using virtual screening

IG Tikhonova, CS Sum, S Neumann… - Journal of medicinal …, 2008 - ACS Publications
The G-protein-coupled receptor free fatty acid receptor 1 (FFAR1), previously named GPR40,
is a possible novel target for the treatment of type 2 diabetes. In an attempt to identify new …

[HTML][HTML] Selective orthosteric free fatty acid receptor 2 (FFA2) agonists: identification of the structural and chemical requirements for selective activation of FFA2 versus …

…, NJ Smith, E Christiansen, IG Tikhonova… - Journal of Biological …, 2011 - ASBMB
Free fatty acid receptor 2 (FFA2; GPR43) is a G protein-coupled seven-transmembrane
receptor for short-chain fatty acids (SCFAs) that is implicated in inflammatory and metabolic …

[HTML][HTML] Identification of residues important for agonist recognition and activation in GPR40

CS Sum, IG Tikhonova, S Neumann, S Engel… - Journal of Biological …, 2007 - ASBMB
GPR40 was formerly an orphan G protein-coupled receptor whose endogenous ligands have
recently been identified as free fatty acids (FFAs). The receptor, now named FFA receptor 1…

[HTML][HTML] Defining the molecular basis for the first potent and selective orthosteric agonists of the FFA2 free fatty acid receptor

…, R Marquez, IG Tikhonova, T Ulven, G Milligan - Journal of Biological …, 2013 - ASBMB
FFA2 is a G protein-coupled receptor that responds to short chain fatty acids and has
generated interest as a therapeutic target for metabolic and inflammatory conditions. However, …

Bidirectional, iterative approach to the structural delineation of the functional “chemoprint” in GPR40 for agonist recognition

IG Tikhonova, CS Sum, S Neumann… - Journal of medicinal …, 2007 - ACS Publications
GPR40, free fatty acid receptor 1 (FFAR1), is a member of the GPCR superfamily and a
possible target for the treatment of type 2 diabetes. In this work, we conducted a bidirectional …

[HTML][HTML] Chemically engineering ligand selectivity at the free fatty acid receptor 2 based on pharmacological variation between species orthologs

BD Hudson, E Christiansen, IG Tikhonova… - The FASEB …, 2012 - ncbi.nlm.nih.gov
When it is difficult to develop selective ligands within a family of related G-protein-coupled
receptors (GPCRs), chemically engineered receptors activated solely by synthetic ligands (…

[HTML][HTML] Old drug, new target: ellipticines selectively inhibit RNA polymerase I transcription

…, T Panova, C Normand, O Gadal, IG Tikhonova… - Journal of Biological …, 2013 - ASBMB
Transcription by RNA polymerase I (Pol-I) is the main driving force behind ribosome biogenesis,
a fundamental cellular process that requires the coordinated transcription of all three …

Extracellular loop 2 of the free fatty acid receptor 2 mediates allosterism of a phenylacetamide ago-allosteric modulator

…, C Tränkle, IG Tikhonova, DR Adams, G Milligan - Molecular …, 2011 - ASPET
Allosteric agonists are powerful tools for exploring the pharmacology of closely related G
protein-coupled receptors that have nonselective endogenous ligands, such as the short chain …

β-Arrestin-dependent and-independent endosomal G protein activation by the vasopressin type 2 receptor

C Daly, AA Guseinov, H Hahn, A Wright, IG Tikhonova… - Elife, 2023 - elifesciences.org
This is an important study that contributes to our understanding of the role of beta-arrestins in
endosomal activation of the vasopressin type 2 receptors. While the use of a minigene as a …